2019-09-15T16:33:42Zhttp://tips.sums.ac.ir/?_action=export&rf=summon&issue=49662017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Cytotoxic evaluation of some new and potent azole derivatives as antimicrobial agentsZeinabFaghihZahraRezaeiAkramJamshidzadehZahraFaghihNaserHeidariSoghraKhabnadidehRecently use of antifungal drugs in human medicine has been increased, especially with the advent of AIDS epidemic. Despite the growing list of azoles, their clinical value has been limited by their relatively high risk of toxicity and the emergence of drug resistance. Efforts have focused on the development of new, less toxic and more efficacious antifungal agents. We previously described synthesis of some new azole derivatives. We also evaluated all the synthesized compounds for their antifungal activity. Most of our compounds showed desirable activity against different species of microorganisms. Here we choose thirteen of these compounds, 5 bentriazole derivatives (1a-5a), 5 imidazole derivatives (1b-5b) and 3 triazole derivatives (1c-3c) to evaluate their cytotoxic activities against a human cancer cell line (MCF-7) using colorimetric MTT cytotoxic assay. Their cytotoxic activities were compared to clotrimazole as a positive control. Our results collectively showed that most of our synthesized compounds had less cytotoxicity against MCF-7 compared to clotrimazole. AzoleAntifungalMTT assayMCF-7 cell line20170901143148http://tips.sums.ac.ir/article_42228_0a150c51e6a1ed574d93f0d1ee433439.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Carnosine Supplementation Mitigates Brain Tissue Markers of Oxidative Stress in a Rat Model of Fulminant Hepatic FailureAkramJamshidzadehNargesAbdoliHosseinNiknahadNegarAzarpiraSomayehMousaviElnazMardaniMojganAbasvaliRezaHeidariFulminant hepatic failure is a deleterious clinical complication, which leads to hyperammonemia. Ammonia is a noxious neurotoxic agent, which affects brain tissue through different mechanisms. On the other hand, it is well-known that oxidative stress and its consequences play a major role in the pathogenesis of ammonia-induced brain injury. Carnosine is a dipeptide abundantly found in the human central nervous system (CNS). This peptide is widely investigated for its neuroprotective properties. The current study aimed to evaluate the effect of carnosine supplementation on oxidative stress markers in the brain tissue of a rat model of fulminant hepatic failure and hyperammonemia. Animals received thioacetamide (400 mg/kg, i.p, for three consecutive days at 24-hr intervals) as a model of acute liver failure and hyperammonemia. Several serum biochemical parameters, in addition to plasma and brain ammonia level, were monitored. On the other hand, brain tissue markers of oxidative stress including reactive oxygen species (ROS) formation, lipid peroxidation, tissue glutathione content, and total antioxidant capacity were measured. It was found that plasma and brain ammonia was increased, and serum markers of liver injury were significantly elevated in the thioacetamide-treated group. On the other hand, an increase in markers of oxidative stress, including ROS formation, lipid peroxidation, glutathione depletion, and decreased tissue antioxidant capacity, was evident in the brain of thioacetamide-treated animals. It was found that carnosine supplementation (250, 500, and 1000 mg/kg) decreased serum markers of liver injury, mitigated brain, and plasma ammonia level, and alleviated brain tissue markers of oxidative stress. These data suggest carnosine as a potential neuroprotective agent with therapeutic capability against ammonia-induced CNS injury.20170901149160http://tips.sums.ac.ir/article_42229_20aa1d67761b2d186e0daf03e741a320.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Captopril fast disintegrating tablets for children: formulation and quality control by HPLCShohrehAlipourAsiyehMohammadiFatemehAhmadiCaptopril is an angiotensin converting enzyme inhibitor, which is used in hypertensive crises and heart failures as an emergency medication especially in pediatrics. Due to difficulty in swallowing of tablets and capsules, pediatric compliance for medication usage is a big challenge in formulation. Considering captopril instability in oral liquid media, it should be formulated as a solid dosage form. Using fast disintegrating tablets (FDTs) is an attractive strategy for solving this problem. According to captopril ultra violet absorption spectrum, high performance liquid chromatography (HPLC) seems to be an accurate, reproducible, and precise method for analysis. Captopril HPLC method was developed and validated for linearity, accuracy, and precision. Because of captopril unacceptable taste especially for children, Eudragit E was used as a taste masking polymer to prepare granules. Crospovidon and Ac-Di-Sol were used as super-disintegrants to reduce tablet disintegration time. Flavoring agents are important ingredients in formulating FDTs for children. Different FDT formulations were prepared by direct compression and granulation-compression method. Quality test of tablets such as thickness, weight, friability, hardness, disintegration time, dissolution profile, and taste masking power were also examined. HPLC validation was confirmed by r2=0.9994, accuracy of 97.4 ± 2.3%, and inter and intra-day precisions of 97.6±1.2 and 97.3± 2.1, respectively. The optimized tablets showed suitable friability (0.85%), hardness (4.1N), and disintegration time (40 sec) with a desirable taste related to presence of Eudragit E. An appropriate and complete dissolution profile within 30 min was also achieved. Results confirmed that captopril taste-masked FDTs would be a pleasant alternative for the available tablets in the market for using in children.20170901161168http://tips.sums.ac.ir/article_42230_2c82c39a758715852b6e0c3f58a8b676.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Myeloprotective effect of Triticum aestivum Linn. grass against antineoplastic agents induced bone marrow toxicity in miceAshishkumarKyadaPankajChoraiMyelotoxicity remains the most important cause of life threatening complications in patients undergoing antineoplastic chemotherapy cycles. Strategies to circumvent or lessen myelotoxicity may improve clinical outcome and quality of life in these patients. The aim of the present study is to investigate myeloprotective effect of Triticum aestivum Linn. (wheat) grass against chemotherapeutic agents induced bone marrow toxicity. Swiss albino mice were pretreated with wheatgrass juice at a dose of 20 ml/kg b.w. for 30 days. An hour after the last dose administration of WGJ, animals were injected with a single i.p. dose of cyclophosphamide (50 mg/kg b.w.) and doxorubicin (50 mg/kg b.w.). The reference drug amifostine (350 mg/kg b.w.) was administered 45 min prior to the cyclophosphamide and doxorubicin injection. At 24 h post chemotherapeutics challenge, animals were euthanized after blood sample collection and bone marrow was aspirated from both femurs. Hematologic parameters in blood samples were measured. Chromosomal abnormalities such as chromatid break, chromosomal ring, chromatid gap, chromatid exchange, chromosome break and number of micronucleated polymorphonuclear erythrocytes formed and polychromatic erythrocytes/normochromatic erythrocytes ratio were recorded in bone marrow smear. The results of present study show that pretreatment with wheatgrass juice significantly protected against cyclophosphamide and doxorubicin induced hematologic abnormalities and chromosomal damage in bone marrow stem cells due to its vast array of active principles. By virtue of its anticlastogenic and cytoprotective effects, wheatgrass juice might be considered as a promising candidate for adjuvant therapy without compromising efficacy of chemotherapeutic agents.wheatgrassmyelotoxicitygenotoxicitychemotherapeutic agentmicronucleuschromosomal aberration20170901169180http://tips.sums.ac.ir/article_42231_e6079206bc943bebc258352fff0e78c3.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Taurine Alleviates Brain Tissue Markers of Oxidative Stress in a Rat Model of Hepatic EncephalopathyAkramJamshidzadehNargesAbdoliHosseinNiknahadNegarAzarpiraElnazMardaniSomayehMousaviMojganAbasvaliRezaHeidariHepatic encephalopathy (HE) is a serious clinical complication, which could lead to coma and death if not appropriately managed. There is agreement on the predominant role of ammonia in the etiology of HE. Brain is one of the most critical organs affected by ammonia. The critical role of oxidative stress and its consequences in the pathogenesis of ammonia-induced brain injury have been revealed before. On the other hand, there is no promising therapeutic option against ammonia neurotoxicity. Taurine is one of the most abundant amino acids in the human body. Several pharmacological roles including brain protecting properties have been attributed to this amino acid. The current study was designed to evaluate the role of taurine supplementation on HE-induced oxidative stress in the brain tissue. Animals received thioacetamide (400 mg/kg, i.p, for three consecutive days at 24-hr intervals) as a model of acute liver failure and hyperammonemia. Several serum biochemical parameters, in addition to plasma and brain ammonia level, were monitored. Moreover, markers of oxidative stress in the brain of hyperammonemic animals were assessed. It was found that plasma and brain ammonia was increased, and serum markers of liver injury were significantly elevated in the thioacetamide-treated group. On the other hand, an increase in markers of oxidative stress, including reactive oxygen species formation, lipid peroxidation, glutathione depletion, and decreased tissue antioxidant capacity, was detected in the brain tissue of thioacetamide-treated animals. It was found that taurine treatment (250, 500, and 1000 mg/kg, i.p) alleviated brain tissue markers of oxidative stress and decreased serum biomarkers of liver injury. Furthermore, lower plasma and brain ammonia were detected in taurine-treated animals. These data suggest taurine as a potential protective agent with therapeutic capability against HE-associated central nervous system complications.20170901181192http://tips.sums.ac.ir/article_42232_f0f84e6cd726ffa40947988232ce9693.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Volatile Composition, Antimicrobial and free radical scavenging activities of essential oil and total extract of Helichrysum leucocephalum Boiss.Mohammad AliJahromiShadabDehshahriSaeedForouzandeh SamaniThe present study investigated the composition of essential oil and evaluation antimicrobial and antioxidant of the ethanolic extract of the aerial parts of Helichrysum leucocephalum. Gas chromatography/mass spectrometry (GC/MS) revealed the presence of 43 compounds which represents 96.8% of the total oil. Carvacrol (20.36%), acetophenone (11.17%) and azulene (7.09%) were identified as the main principal components of the essential oil. H. leucocephalum ethanolic extract exhibited a high phenol content (114.13±0.89 mg gallic acid equivalent (GAE)/g of dry plant) while total flavonoid content was found to be 43.26±0.70 mg quercetin equivalent (QE)/g of dry plant). In order to evaluate antioxidant efficacy of the essential oil and ethanolic extract, DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging and ferric reducing antioxidant power. (FRAP) assays were conducted. The ethanolic extract demonstrated significant DPPH free radical Inhibitory activity (IC50 = 61.35±0.07 µg/mL) and ferric reducing ability (IC50= 113.43±0.58 µg/mL) while the essential oil declared a weak antioxidant properties. Antimicrobial screening revealed higher degree of inhibition for essential oil of the aerial parts of H. leucocephalum against Staphylococcus aureus and Escherichia coli both with MIC value, 16 µg/mL. Additionally the essential oil of H. leucocephalum exhibited antifungal properties when tested against Candida albicans (MIC50, 32 µg/mL). 20170901193200http://tips.sums.ac.ir/article_42233_eea30b907e8ba0617ffda355f0d59647.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733The effects of saffron consumption on lipid profile, liver enzymes, and oxidative stress in male hamsters with high fat dietSinaVakiliAmirSavardashtakiMohammad AminMomeni MoghaddamPeymanNowrouziMohammadKhabbaz ShiraziGhasemEbrahimiSaffron (Crocus sativus) is one of the indigenous plants of Iran. Recently its possible effects have been reported on lipid abnormalities and oxidative stress. The aim of this study was to investigate the effects of saffron consumption on lipid profiles, especially the reduction of blood cholesterol, and lipid peroxidation in male hamsters under a high-fat diet. Twenty-six hamster rats were categorized in control group, high-fat diet group (HFD), and high-fat diet group treated with an aqueous saffron extract (HFD+S). The HFD and HFD+S groups were subjected to high-fat diet for 30 days. During last 10 days of this course, the HFD+S group received 100 mg/kg/day saffron through gavage. Saffron administration along with a high fat diet significantly decreased serum levels of total cholesterol, low molecular weight lipoprotein (LDL) cholesterol, malondialdehyde (MDA), and some hepatic enzymes. These results support the possible effects of saffron consumption in the prevention and treatment of cardiovascular disease.CrocusCardiovascular diseaseLipidsLiverMalondialdehydeProtein carbonylationHigh-fat diet20170901201208http://tips.sums.ac.ir/article_42234_0241d8a616cd6cc75936c1d10ca82d37.pdf2017-09-0110.30476Trends in Pharmaceutical Sciences2423-37222423-3722201733Fatal cases of strychnine ingestion referred to Fars Legal Medicine Organization; Autopsy findings and Analytical methods used in strychnine detectionMaryamHosseiniAbdorrasoulMalekpourRezaKhoshnoudHasanAbbasiniaSaeidGholamzadehTaherehTarianAsiyehHashemiStrychnine is a toxic alkaloid which might be the source of poisoning with homicidal and suicidal purposes. Eleven fatal cases of strychnine ingestion were considered in this study. Strychnine was isolated from biological samples using the solid phase extraction (SPE) procedure and detected by analytical methods such as thin layer chromatography (TLC), gas chromatography/mass spectrometry (GC-MS) as well as high performance liquid chromatography (HPLC). Eleven cases of strychnine ingestion including 8 men and 3 women with minimum and maximum ages of 17 and 56 years old have been studied. Most of them had an education level of high school and had neither criminal history nor psychological disorders except for 3 cases that were using psychiatric drugs. Facial and ocular congestion, facial cyanosis, lung edema and hemorrhage were found in all of the cases. Hyperemic kidney, brain, liver and meninges and lung collapse were other pathologic findings encountered. Reactive gliosis, subarachnoid focal hemorrhage and 6 cm laceration on the left side of the face were separately found in three cases. Considering highly fatal effects of strychnine and its potential suicidal use, it should be strictly and severely prohibited and watched out for its misuse. On the other hand, the analytical methods used, indicated their reliable, simple, specific and sensible application in forensic and clinical investigations.Fatal ingestionGC-MSSolid Phase ExtractionStrychnine20170901209214http://tips.sums.ac.ir/article_42235_34a9cb8c23c11a1ff978b301615c9f46.pdf